Target Information

Target General Infomation
Target ID
T75984
Former ID
TTDI01743
Target Name
5-HT 2 receptor
Target Type
Successful
Disease Alcohol use disorders [ICD9: 303; ICD10: F10.2]
Arthritis [ICD9: 710-719; ICD10: M00-M25]
Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
Cerebrovascular ischaemia [ICD9: 434.91; ICD10: I61-I63]
Depression [ICD9: 311; ICD10: F30-F39]
Generalized anxiety disorder; Social phobia [ICD9: 300, 300.02, 300.23; ICD10: F40-F42, F40.1, F41.1, F93.2]
Hypertension [ICD9: 401; ICD10: I10-I16]
Migraine [ICD9: 346; ICD10: G43]
Psychotic disorders [ICD9: 290-299; ICD10: F20-F29]
Peripheral vascular disease [ICD9: 443.9; ICD10: I73.9]
Schizophrenia [ICD9: 295; ICD10: F20]
Thromboembolism [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82]
Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5- dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling activates phospholipase C and a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and promotes the release of Ca(2+) ions from intracellular stores. Affects neural activity, perception, cognition and mood. Plays a role in the regulation of behavior, including responses to anxiogenic situations and psychoactive substances. Plays a role in intestinal smooth muscle contraction, and may play a role in arterial vasoconstriction.
Drugs and Mode of Action
Drug(s) Perospirone Drug Info Approved Psychotic disorders [542556], [551871]
Bis(olanzapine) pamoate monohydrate Drug Info Phase 3 Psychotic disorders [551871]
FK949E Drug Info Phase 3 Alcohol use disorders [525091]
Nexopamil Drug Info Phase 2 Hypertension [533605]
TGOF02N Drug Info Phase 2 Schizophrenia [550649]
TGWOOAA Drug Info Phase 2 Generalized anxiety disorder; Social phobia [550646]
AMAP-102 Drug Info Phase 1 Arthritis [522820]
ICI-170809 Drug Info Discontinued in Phase 2 Anxiety disorder [544978]
SUN-C5174 Drug Info Discontinued in Phase 2 Peripheral vascular disease [547072]
Beloxepin Drug Info Discontinued in Phase 1 Depression [544856]
SUN-9221 Drug Info Discontinued in Phase 1 Hypertension [546178]
AHR-16303B Drug Info Terminated Hypertension [528509]
Dotarizine Drug Info Terminated Migraine [525748]
E-2040 Drug Info Terminated Schizophrenia [546598]
Emopamil Drug Info Terminated Cerebrovascular ischaemia [534257]
MDL-28133A Drug Info Terminated Thromboembolism [545319]
NPC-18166 Drug Info Terminated Psychotic disorders [545751]
Modulator AHR-16303B Drug Info [528509]
Beloxepin Drug Info [550142]
Bis(olanzapine) pamoate monohydrate Drug Info [551871]
Dotarizine Drug Info [525748]
E-2040 Drug Info [546599]
Emopamil Drug Info [534257]
FK949E Drug Info [526036], [534577]
ICI-170809 Drug Info [533671]
MDL-28133A Drug Info [533621]
Nexopamil Drug Info [533605]
NPC-18166 Drug Info [550952]
Perospirone Drug Info [533697], [551871]
SUN-9221 Drug Info [525435]
TGOF02N Drug Info [550648]
Antagonist AMAP-102 Drug Info [549726]
SUN-C5174 Drug Info [525776]
TGWOOAA Drug Info [550645]
Pathways
KEGG Pathway Calcium signaling pathway
Neuroactive ligand-receptor interaction
Gap junction
Serotonergic synapse
Inflammatory mediator regulation of TRP channels
References
Ref 522820ClinicalTrials.gov (NCT00995605) AMAP102 - Safety, Tolerability and Pharmacokinetics in Healthy Subjects. U.S. National Institutes of Health.
Ref 525091ClinicalTrials.gov (NCT02362412) Study to Evaluate the Effects of Switching Different Strength Forms of FK949E in Bipolar Disorder Patients With Major Depressive Episodes. U.S. National Institutes ofHealth.
Ref 525748Vasostabilizing effect of Dotarizine (Ca(2+)-channel blocker) on cerebrovascular reactivity in rabbits. Neurol Res. 2000 Mar;22(2):229-32.
Ref 528509AHR-16303B, a novel antagonist of 5-HT2 receptors and voltage-sensitive calcium channels. J Cardiovasc Pharmacol. 1991 Jan;17(1):41-53.
Ref 533605Inhibition by the combined Ca2+ and 5-HT2 receptor antagonist nexopamil (LU 49938) of intracoronary thrombus formation in a canine model of arterial stenosis and intimal damage. J Cardiovasc Pharmacol. 1993 Nov;22(5):687-94.
Ref 534257Calcium entry and 5-HT2 receptor blockade in oliguric ischaemic acute renal failure: effects of levemopamil in conscious rats. Br J Pharmacol. 1996 Mar;117(6):1348-54.
Ref 542556(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7556).
Ref 544856Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001334)
Ref 544978Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001766)
Ref 545319Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002814)
Ref 545751Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004563)
Ref 546178Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006767)
Ref 546598Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009126)
Ref 547072Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012828)
Ref 550646Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals.
Ref 550649Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525435Synthesis and pharmacological evaluation of pyrroloazepine derivatives as potent antihypertensive agents with antiplatelet aggregation activity. Chem Pharm Bull (Tokyo). 1999 Feb;47(2):246-56.
Ref 525748Vasostabilizing effect of Dotarizine (Ca(2+)-channel blocker) on cerebrovascular reactivity in rabbits. Neurol Res. 2000 Mar;22(2):229-32.
Ref 525776Synthesis and serotonin 2 (5-HT2) receptor antagonist activity of 5-aminoalkyl-substituted pyrrolo[3,2-c]azepines and related compounds. Chem Pharm Bull (Tokyo). 2000 May;48(5):623-35.
Ref 526036D(2) and 5HT(2A) receptor occupancy of different doses of quetiapine in schizophrenia: a PET study. Eur Neuropsychopharmacol. 2001 Apr;11(2):105-10.
Ref 528509AHR-16303B, a novel antagonist of 5-HT2 receptors and voltage-sensitive calcium channels. J Cardiovasc Pharmacol. 1991 Jan;17(1):41-53.
Ref 533605Inhibition by the combined Ca2+ and 5-HT2 receptor antagonist nexopamil (LU 49938) of intracoronary thrombus formation in a canine model of arterial stenosis and intimal damage. J Cardiovasc Pharmacol. 1993 Nov;22(5):687-94.
Ref 533621Effects of MDL 28,133A, a 5-HT2 receptor antagonist, on platelet aggregation and coronary thrombosis in dogs. J Cardiovasc Pharmacol. 1994 Nov;24(5):761-72.
Ref 5336715-HT2 receptor blockade by ICI 170,809 does not affect the inhibitory effect of the 5-HT1A receptor ligand gepirone on neuroleptic-induced catalepsy. Braz J Med Biol Res. 1994 Oct;27(10):2437-41.
Ref 533697Pharmacological effects of zotepine and other antipsychotics on the central 5-HT2 receptors. Pharmacopsychiatry. 1993 Mar;26(2):53-8.
Ref 534257Calcium entry and 5-HT2 receptor blockade in oliguric ischaemic acute renal failure: effects of levemopamil in conscious rats. Br J Pharmacol. 1996 Mar;117(6):1348-54.
Ref 534577Time course of central nervous dopamine-D2 and 5-HT2 receptor blockade and plasma drug concentrations after discontinuation of quetiapine (Seroquel) in patients with schizophrenia. Psychopharmacology(Berl). 1998 Jan;135(2):119-26.
Ref 546599Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009126)
Ref 549726Clinical pipeline report, company report or official report of Anamar.
Ref 550142WO patent application no. 2009,1055,07, Beloxepin, its enantiomers, and analogs thereof for the treatment of pain.
Ref 550645Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals.
Ref 550648Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals.
Ref 550952WO patent application no. 2004,0825,84, 5ht2c receptor antagonists in the treatment of schizophrenia.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

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